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Assay Detail

CHEMBL5543896

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Binding
Inhibition of ovine COX-1 by colorimetric assay
26
Total Activities
26
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Ovis aries
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Prostaglandin G/H synthase 1 (CHEMBL2949)
Type SINGLE PROTEIN
Organism Ovis aries

Publication

A further pocket or conformational plasticity by mapping COX-1 catalytic site through modified-mofezolac structure-inhibitory activity relationships and their antiplatelet behavior.
Solidoro R, Miciaccia M, Bonaccorso C, Fortuna CG, Armenise D, Centonze A, Ferorelli S, Vitale P, Rodrigues P, Guimarães R, de Oliveira A, da Paz M, Rangel L, Sathler PC, Altomare A, Perrone MG, Scilimati A.
Eur J Med Chem (2024) 266 : 116135 -116135
PubMed 38219659 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 26 6.92 8.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL259972 MOFEZOLAC 4.0 1 8.10
CHEMBL5573862 1 7.34
CHEMBL5567378 1 7.28
CHEMBL4462870 1 7.12
CHEMBL5572914 1 7.10
CHEMBL5572619 1 6.92
CHEMBL5572292 1 6.92
CHEMBL5569710 1 6.64
CHEMBL5573040 1 6.50
CHEMBL5579661 1 6.35
CHEMBL5571714 1 5.89
CHEMBL5563480 1 -
CHEMBL5574653 1 -
CHEMBL5593821 1 -
CHEMBL5583683 1 -
CHEMBL5573058 1 -
CHEMBL5571322 1 -
CHEMBL5591112 1 -
CHEMBL5563326 1 -
CHEMBL5591549 1 -
CHEMBL5564783 1 -
CHEMBL5569519 1 -
CHEMBL5570107 1 -
CHEMBL5575442 1 -
CHEMBL5595152 1 -
CHEMBL5564448 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL259972 MOFEZOLAC IC50 = 8.0 nM 8.10
CHEMBL5573862 IC50 = 46.0 nM 7.34
CHEMBL5567378 IC50 = 53.0 nM 7.28
CHEMBL4462870 IC50 = 76.0 nM 7.12
CHEMBL5572914 IC50 = 79.0 nM 7.10
CHEMBL5572619 IC50 = 120.0 nM 6.92
CHEMBL5572292 IC50 = 120.0 nM 6.92
CHEMBL5569710 IC50 = 230.0 nM 6.64
CHEMBL5573040 IC50 = 320.0 nM 6.50
CHEMBL5579661 IC50 = 450.0 nM 6.35
CHEMBL5571714 IC50 = 1300.0 nM 5.89
CHEMBL5563480 IC50 > 50000.0 nM -
CHEMBL5574653 IC50 > 50000.0 nM -
CHEMBL5593821 IC50 > 50000.0 nM -
CHEMBL5583683 IC50 > 50000.0 nM -
CHEMBL5573058 IC50 > 50000.0 nM -
CHEMBL5571322 IC50 > 50000.0 nM -
CHEMBL5591112 IC50 > 50000.0 nM -
CHEMBL5563326 IC50 > 50000.0 nM -
CHEMBL5591549 IC50 > 50000.0 nM -
CHEMBL5564783 IC50 > 50000.0 nM -
CHEMBL5569519 IC50 > 50000.0 nM -
CHEMBL5570107 IC50 > 50000.0 nM -
CHEMBL5575442 IC50 > 50000.0 nM -
CHEMBL5595152 IC50 > 50000.0 nM -
CHEMBL5564448 IC50 > 50000.0 nM -